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Synthesis of 5-(2,3-ditritiopropoxy)-3-(1,2,5,6-tetrahydropyrid-4-yl)indole ([3H]CP-96,501): A selective ligand for the serotonin (5-HT1B) receptor

✍ Scribed by John E. Macor; Carol A. Burkhart; Lorraine A. Lebel; B. Kenneth Koe; Phillip M. Chalabi; James C. Windels; Robert W. Roth

Publisher: John Wiley and Sons
Year: 1991
Tongue: French
Weight: 431 KB
Volume: 29
Category: Article
ISSN: 0022-2135
DOI: 10.1002/jlcr.2580290302

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✦ Synopsis

Abstract

The synthesis of [^3^H]CP‐96,501 [5‐(2,3‐ditritiopropoxy)‐3‐(1,2,5,6‐tetrahydropyrid‐4‐yl)indole], a selective radioligand for the serotonin (5‐HT~1B~) receptor and analog of RU‐24,969, is described. 5‐Hydroxyindole is converted in two steps to 5‐(2‐propenyloxy)‐3‐(N‐t‐butoxycarbonyl‐1,2,5,6‐tetrahydropyrid‐4‐yl)indole (3). Hydrogena‐tion or tritiation of 3 followed by removal of the t‐butoxycarbonyl protecting group afforded CP‐96,501 (1a) and [^3^H] CP‐96,501 (1b), respectively.

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